PQR-530 |
Catalog No.GC33385 |
Le PQR-530 est un inhibiteur double pan-PI3K/mTORC1/2 puissant, compétitif pour l'ATP, biodisponible par voie orale et pénétrant dans le cerveau, avec un Kd sous-nanomolaire vers PI3Kα et mTOR (0,84 et 0,33 nM, respectivement). Activité antitumorale.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1927857-61-1
Sample solution is provided at 25 µL, 10mM.
PQR-530 is a potent, oral and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, exhibiting antitumor activity.
PQR-530 is a potent, oral and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, exhibiting antitumor activity. PQR-530 inhibits all PI3K isoforms and mTOR complexes C1/2 potently and selectively. PQR-530 inhibits protein kinase B (PKB, pSer473) and ribosomal protein S6 (pS6, pSer235/236) phosphorylation with IC50 values of 0.07 µM in A2058 melanoma cells. PQR-530 shows inhibitory activity against the growth of 44 cancer cell lines with mean GI50 of 426 nM[1].
[1]. Denise Rageot, et al. Abstract 140: Discovery and biological evaluation of PQR530, a highly potent dual pan-PI3K/mTORC1/2 inhibitor. Cancer Res 2017;77(13 Suppl).
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